Fear God (UNDER CONSTRUCTION)

FEAR GOD

Revelation 14: 7 And I saw another angel fly in the midst of heaven, having the everlasting gospel to preach unto them that dwell on the earth, and to every nation, and kindred, and tongue, and people, 7Saying with a loud voice, Fear God, and give glory to him; for the hour of his judgment is come: and worship him that made heaven, and earth, and the sea, and the fountains of waters. 8And there followed another angel, saying, Babylon is fallen, is fallen, that great city, because she made all nations drink of the wine of the wrath of her fornication. 8And there followed another angel, saying, Babylon is fallen, is fallen, that great city, because she made all nations drink of the wine of the wrath of her fornication. 9And the third angel followed them, saying with a loud voice, If any man worship the beast and his image, and receive his mark in his forehead, or in his hand, 10The same shall drink of the wine of the wrath of God, which is poured out without mixture into the cup of his indignation; and he shall be tormented with fire and brimstone in the presence of the holy angels, and in the presence of the Lamb: 11And the smoke of their torment ascendeth up for ever and ever: and they have no rest day nor night, who worship the beast and his image, and whosoever receiveth the mark of his name. 12Here is the patience of the saints: here are they that keep the commandments of God, and the faith of Jesus.

Ecclesiastes 12:13 Let us hear the conclusion of the whole matter: Fear God, and keep his commandments: for this is the whole duty of man.14For God shall bring every work into judgment, with every secret thing, whether it be good, or whether it be evil.

Universality and Cosmology

ANALYZING UNDERLYING IMPETUSES AS REFLECTED IN HISTORY (1840's-present)
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Universitarianism reflected in religions, military, and politics. (1800's) III

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Sunday, November 14, 2010

Pregabalin (Lyrica)

Pregabalin

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Pregabalin
Systematic (IUPAC) name
(S)-3-(aminomethyl)-5-methylhexanoic acid
Identifiers
CAS number 148553-50-8
ATC code N03AX16
PubChem CID 5486971
DrugBank APRD01198
ChemSpider 4589156
UNII 55JG375S6M
Chemical data
Formula C8H17NO2 
Mol. mass 159.23 g.mol-1
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability ≥90%
Protein binding Nil
Metabolism Negligible
Half-life 5–6.5 hours
Excretion Renal
Therapeutic considerations
Licence data US Daily Med:link
Pregnancy cat. B3 (Au), C (U.S.)
Legal status S4 (Au), POM (UK), Schedule V (U.S.)
Routes Oral(main), IV, Insufflation
 YesY(what is this?)  (verify)
Pregabalin (INN) (pronounced /prɨˈɡæbəlɨn/) is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults.[1] It has also been found effective for generalized anxiety disorder and is (as of 2007) approved for this use in the European Union.[1] It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica.
Recent studies have shown that pregabalin is effective at treating chronic pain in disorders such as fibromyalgia[2] and spinal cord injury.[3] In June 2007, pregabalin became the first medication approved by the U.S. Food and Drug Administration specifically for the treatment of fibromyalgia.[4]
It is considered to have a low potential for abuse, and a limited dependence liability if misused, and is thus classified as a Schedule V drug in the U.S.[5]
Lyrica is one of four drugs which a subsidiary of Pfizer in 2009 pleaded guilty to misbranding "with the intent to defraud or mislead". Pfizer agreed to pay $2.3 billion (£1.4 billion) in settlement, and entered a corporate integrity agreement. Pfizer illegally promoted the drugs and caused false claims to be submitted to government healthcare programs for uses that were not medically accepted.[6]
Pregabalin is available in 25, 50, 75, 100, 150, 200, 225, and 300 mg capsules, and recently a strawberry flavoured oral solution has been developed, containing 20mg/mL with an added sweetening agent (sucrose) to mask the chemical's bitter taste.[7][8]

Contents

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[edit] History

Pregabalin was initially developed by medicinal chemist Richard Bruce Silverman at Northwestern University in the United States. The drug was approved in the European Union in 2004. Pregabalin received U.S. Food and Drug Administration (FDA) approval for use in treating epilepsy, diabetic neuropathic pain, and post-herpetic neuralgia in December 2004, and appeared on the U.S. market in fall 2005.[9]
In June 2007, the FDA approved Lyrica as a treatment for fibromyalgia. It was the first drug to be approved for this indication and remained the only one until duloxetine (Cymbalta) gained FDA approval for the treatment of fibromyalgia in June 2008.[10]

[edit] Indications

Pregabalin is indicated for:
Its therapeutic effect appears after 1 week of use and is similar in effectiveness to lorazepam, alprazolam and venlafaxine but pregabalin has demonstrated superiority by producing more consistent therapeutic effects for psychic and somatic anxiety symptoms. Long-term trials have shown continued effectiveness without the development of tolerance and additionally unlike benzodiazepines it does not disrupt sleep architecture and produces less severe cognitive and psychomotor impairment; it also has a low potential for abuse and dependence and may be preferred over the benzodiazepines for these reasons.[13][14]
It has not been found to be effective for HIV-associated peripheral neuropathy.[15]

[edit] Adverse effects

Adverse drug reactions associated with the use of pregabalin include:[16][17]
Pregabalin may also cause withdrawal effects after long-term use if discontinued abruptly. When prescribed for seizures, quitting "cold turkey" can increase the strength of the seizures and possibly cause the seizures to reoccur. Withdrawal symptoms include restlessness, insomnia, and anxiety. Pregabalin should be reduced gradually when finishing treatment.[citation needed]

[edit] Overdosage

Several renal failure patients developed myoclonus while receiving pregabalin, appparently as a result of gradual accumulation of the drug. Acute overdosage may be manifested by somnolence, tachycardia and hypertonicity. Plasma, serum or blood concentrations of pregabalin may be measured to monitor therapy or to confirm a diagnosis of poisoning in hospitalized patients.[19][20][21]

[edit] Pharmacology

[edit] Pharmacodynamics

Like gabapentin, pregabalin binds to the α2δ (alpha2delta) subunit of the voltage-dependent calcium channel in the central nervous system. This reduces calcium influx into the nerve terminals. Pregabalin also decreases the release of neurotransmitters such as glutamate, noradrenaline, and substance P (Australian Medicines Handbook). Pregabalin increases neuronal GABA levels by producing a dose-dependent increase in glutamic acid decarboxylase activity.[1] Glutamic acid decarboxylase (GAD) is the enzyme that converts the excitatory neurotransmitter glutamate into the inhibitory GABA in a single step. For this reason, pregabalin greatly potentiates benzodiazepines, barbiturates & other depressants.

[edit] Pharmacokinetics

Absorption: Pregabalin is rapidly absorbed when administered on an empty stomach, with peak plasma concentrations occurring within one hour. Pregabalin oral bioavailability is estimated to be greater than or equal to 90% and is independent of dose. The rate of pregabalin absorption is decreased when given with food resulting in a decrease in Cmax by approximately 25 to 30% and a delay in Tmax to approximately 2.5 hours. Administration with food, though, has no clinically significant effect on the extent of absorption.[22]
Distribution: Pregabalin has been shown to cross the blood-brain barrier in mice, rats, and monkeys. Pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats. In humans, the volume of distribution of pregabalin for an orally administered dose is approximately 0.56 L/kg and is not bound to plasma proteins.[22]
Metabolism: Pregabalin undergoes negligible metabolism in humans.[23] Approximately 98% of the radioactivity recovered in the urine was unchanged pregabalin. The N-methyl pregabalin is the major metabolite.[22]
Excretion: Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug.[22] Renal clearance of pregabalin is 73 mL/minute.[verification needed]

[edit] Drug interactions

No pharmacokinetic interactions have been demonstrated in vivo. The manufacturer notes some potential pharmacological interactions with opioids (pregabalin is synergistic with opioids in lower doses), benzodiazepines, barbiturates, ethanol (alcohol), and other drugs that depress the central nervous system.[16]

[edit] Misuse

Pregabalin is a Schedule V drug, classified as a CNS depressant. The potential for abuse of pregabalin is significantly less than the potential with benzodiazepines.[24]

[edit] References

  1. ^ a b Benkert, O., Hippius, H. et al.: Kompendium der Psychiatrischen Pharmakotherapie, 6. Auflage, Springer Medizin Verlag, Heidelberg, 2007. (german) ISBN 9783540344018
  2. ^ Crofford LJ, Rowbotham MC, Mease PJ, et al. (2005). "Pregabalin for the treatment of fibromyalgia syndrome: results of a randomized, double-blind, placebo-controlled trial". Arthritis Rheum 52 (4): 1264–73. doi:10.1002/art.20983. PMID 15818684.  Free full text
  3. ^ Siddall PJ, Cousins MJ, Otte A, Griesing T, Chambers R, Murphy TK (2006). "Pregabalin in central neuropathic pain associated with spinal cord injury: a placebo-controlled trial". Neurology 67 (10): 1792–800. doi:10.1212/01.wnl.0000244422.45278.ff. PMID 17130411. 
  4. ^ U.S. Food and Drug Administration (June 21, 2007). "FDA Approves First Drug for Treating Fibromyalgia". Press release. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2007/ucm108936.htm. Retrieved 2010-10-30. 
  5. ^ Drug Enforcement Administration, Department of Justice. Schedules of controlled substances: placement of pregabalin into schedule V. Final rule. Fed Regist 2005;70(144):43633-5. PMID 16050051
  6. ^ Pfizer agrees record fraud fine
  7. ^ http://www.rxlist.com/lyrica-drug.htm
  8. ^ http://priorartdatabase.com/IPCOM/000187748
  9. ^ Dworkin RH, Kirkpatrick P (June 2005). "Pregabalin" (PDF on free subscription). Nature Reviews Drug Discovery 4 (6): 455–6. doi:10.1038/nrd1756. PMID 15959952. http://www.nature.com/nrd/journal/v4/n6/pdf/nrd1756.pdf. 
  10. ^ http://www.fda.gov/ForConsumers/ConsumerUpdates/ucm107802.htm
  11. ^ "Pfizer's Lyrica Approved for the Treatment of Generalized Anxiety Disorder (GAD) in Europe". Press release. http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/03-27-2006/0004327379. Retrieved 2007-07-04. 
  12. ^ Bandelow, B.; Wedekind, D.; Leon, T. (Jul 2007). "Pregabalin for the treatment of generalized anxiety disorder: a novel pharmacologic intervention.". Expert Rev Neurother 7 (7): 769–81. doi:10.1586/14737175.7.7.769. PMID 17610384. 
  13. ^ Bandelow, B.; Wedekind, D.; Leon, T. (Jul 2007). "Pregabalin for the treatment of generalized anxiety disorder: a novel pharmacologic intervention.". Expert Rev Neurother 7 (7): 769–81. doi:10.1586/14737175.7.7.769. PMID 17610384. 
  14. ^ Owen, RT. (Sep 2007). "Pregabalin: its efficacy, safety and tolerability profile in generalized anxiety.". Drugs Today (Barc) 43 (9): 601–10. doi:10.1358/dot.2007.43.9.1133188. PMID 17940637. 
  15. ^ Simpson DM, Schifitto G, Clifford DB, et al. (February 2010). "Pregabalin for painful HIV neuropathy: a randomized, double-blind, placebo-controlled trial". Neurology 74 (5): 413–20. doi:10.1212/WNL.0b013e3181ccc6ef. PMID 20124207. 
  16. ^ a b Pfizer Australia Pty Ltd. Lyrica (Australian Approved Product Information). West Ryde: Pfizer; 2006.
  17. ^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
  18. ^ Medication Guide
  19. ^ Murphy NG, Mosher L. Severe myoclonus from pregabalin (Lyrica) due to chronic renal insufficiency. Clin. Tox. 46: 594, 2008.
  20. ^ Yoo L, Matalon D, Hoffman RS, Goldfarb DS. Treatment of pregabalin toxicity by hemodialysis in a patient with kidney failure. Am. J. Kidney Dis. 54: 1127-1130, 2009.
  21. ^ R. Baselt, Disposition of Toxic Drugs and Chemicals in Man, 8th edition, Biomedical Publications, Foster City, CA, 2008, pp. 1296-1297.
  22. ^ a b c d "Summary of product characteristics". European Medicines Agency. 19 August 2009. http://www.emea.europa.eu/humandocs/PDFs/EPAR/lyrica/emea-combined-h546en.pdf. Retrieved 8 September 2009. 
  23. ^ Susan L. McElroy,. Antiepileptic Drugs to Treat Psychiatric Disorders. p. 370. }
  24. ^ Chalabianloo, F; Schjøtt J (January 2009). "Pregabalin and its potential for abuse". Journal of the Norwegian Medical Association 129 (3): 186–187. doi:10.4045/tidsskr.08.0047. PMID 19180163. http://www.tidsskriftet.no/index.php?vp_SEKS_ID=1797598. 

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